Didesmethylchlorpromazine sulfone [gamma-(2-chlorophenothiazinyl-10)-propylamine sulfone] has been isolated from the urine of a patient under continuous chlorpromazine therapy and identified by mass spectrometry. The same compound was present in organs of rats after injection of the corresponding sulfide. The Cl-free analogue, gamma-(phenothiazinyl-10)-propylamine sulfone, was excreted by patients receiving perazine and by a volunteer after ingestion of the primary amine sulfoxide.
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Environ Sci Technol
January 2025
State Key Laboratory of Environmental Chemistry and Ecotoxicology, Research Center for Eco-Environmental Sciences, The Chinese Academy of Sciences, Beijing 100085, P. R. China.
It is well known that hydroxyl radical (OH) can be largely produced either through the classic iron-mediated inorganic-Fenton system or our recently discovered haloquinones/HO organic-Fenton-like system, but rarely produced via thiol compounds. Here, unexpectedly, we found that OH can be unequivocally generated by incubation of HO and mercaptotriazole (MTZ), a typical heterocyclic thiol which has been used as an environmentally friendly corrosion inhibitor for mild steel. By the complementary applications of HPLC-MS and oxygen-18 isotope-labeling method, MTZ-derived sulfenic (MTZ-SOH) and sulfinic acids were detected and identified as transient intermediates, and sulfonic acid as final products.
View Article and Find Full Text PDFBiochemistry (Mosc)
December 2024
Medicinal Chemistry Center, Togliatti State University, Togliatti, 445020, Russia.
Human carbonic anhydrase IX (CAIX) plays a key role in maintaining pH homeostasis of malignant neoplasms, thus creating a favorable microenvironment for the growth, invasion, and metastasis of tumor cells. Recent studies have established that inhibition of CAIX expressed on the surface of tumor cells significantly increases the efficacy of classical chemotherapeutic agents and makes it possible to suppress the resistance of tumor cells to chemotherapy, as well as to increase their sensitivity to drugs (in particular, to reduce the required dose of cytostatic agents). In this work, we studied the ability of new CAIX inhibitors based on substituted 1,2,4-oxadiazole-containing primary aromatic sulfonamides, to potentiate the cytostatic effect of gefitinib (selective inhibitor of epidermal growth factor receptor tyrosine kinase domain) under hypoxic conditions.
View Article and Find Full Text PDFCancer Biol Ther
December 2025
Department of Hematology, Taixing People's Hospital Affiliated to Yangzhou University, Taixing, China.
Objectives: Acute T-cell lymphoblastic leukemia (T-ALL) is a severe hematologic malignancy with limited treatment options and poor long-term survival. This study explores the role of IKZF1 in regulating BCL-2 expression in T-ALL.
Methods: CUT&Tag and CUT&Run assays were employed to assess IKZF1 binding to the BCL-2 promoter.
Molecules
January 2025
Department of Manufacturing Pharmacy, College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan 46241, Republic of Korea.
Fifteen compounds (-) constructed on a hybrid structure combining a β-phenyl-α,β-unsaturated carbonyl template and a 2-aminothiazol-4(5)-one scaffold were designed and synthesized as potential novel anti-tyrosinase substances. Two compounds ( and ) showed more potent inhibition against mushroom tyrosinase than kojic acid, and the inhibitory activity of (IC value: 1.60 μM) was 11 times stronger than that of kojic acid.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Department of Pharmaceutical Biochemistry, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznań, Poland.
Adult-type diffuse gliomas are characterized by inevitable recurrence and very poor prognosis. Novel treatment options, including multimodal drugs or effective drug combinations, are therefore eagerly awaited. Tinostamustine is an alkylating and histone deacetylase inhibiting molecule with great potential in cancer treatment.
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